BI-853520
(Synonyms: IN-10018) 目录号 : GC65886
BI 853520 (IN-10018) 是一种具有口服活性的粘附斑激酶 (FAK) 强效抑制剂 (重组 FAK IC50=1 nM)，BI 853520 表现出对癌细胞的抗增殖活性。
Cas No.:1227948-82-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
BI 853520 (IN-10018) is an orally active and potent focal adhesion kinase (FAK) inhibitor (recombinant FAK IC50=1 nM). BI 853520 shows anti-proliferative activity against cancer cells[1][2].
BI 853520 (0-3 μM; 2 h) inhibits cancer cells growth[2].
BI 853520 (0-30 μM; 4-6 d) represses tumor cell proliferation and invasion only in 3D culture[1].
BI 853520 (0-10 μM; 24 h) represses Y397-FAK autophosphorylation[1].
BI 853520 (0.1 μM; 96 h) shows a fast and potent inhibition of FAK in this highly metastatic murine breast cancer cell line[1].
Cell Viability Assay[2]
| Cell Line: | PC-3 cells |
| Concentration: | 0-3 μM |
| Incubation Time: | 2 hours |
| Result: | Resulted in a concentration-dependent reduction of the signal with a median EC50 value of 1 nM. |
Cell Proliferation Assay[1]
| Cell Line: | 4T1, Py2T, and Py2T-LT cells |
| Concentration: | 0-30 μM |
| Incubation Time: | 4-6 days |
| Result: | Indicated that the specific inhibition of cell proliferation and invasion at low doses is functional only in three-dimensional cell culture conditions, whereas cells cultured on plastic only respond to BI 853520 at very high, toxic doses. |
Western Blot Analysis[1]
| Cell Line: | 4T1, Py2T, and Py2T-LT cells |
| Concentration: | 0-10 μM |
| Incubation Time: | 24 hours |
| Result: | Reduced Y397-FAK autophosphorylation in all cell types. |
Western Blot Analysis[1]
| Cell Line: | 4T1, Py2T, and Py2T-LT cells |
| Concentration: | 0.1 μM |
| Incubation Time: | 96 hours |
| Result: | Decreased Y397-FAK autophosphorylation following 0.1 µM BI 853520 treatment occurred within 10 min and was substantially reduced at least for the following 48 h. |
BI 853520 (oral gavage; 50 mg/kg; once daily; 0-8 weeks) treatment significantly suppresses primary tumor growth of all three cell lines in vivo[1].
| Animal Model: | FVB/N, Balb/c, or immunodeficient nude (nu/nu) mice transplanted with Py2T, 4T1, or MTflECad cells, respectively[1] |
| Dosage: | 50 mg/kg |
| Administration: | Oral gavage; 50 mg/kg; once daily; 0-8 weeks |
| Result: | Decreased tumor volume significantly over time. |
| Cas No. | 1227948-82-4 | SDF | Download SDF |
| 别名 | IN-10018 | ||
| 分子式 | C28H28F4N6O4 | 分子量 | 588.55 |
| 溶解度 | 储存条件 | Store at -20°C | |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.6991 mL | 8.4955 mL | 16.9909 mL |
| 5 mM | 0.3398 mL | 1.6991 mL | 3.3982 mL |
| 10 mM | 0.1699 mL | 0.8495 mL | 1.6991 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Drug Discovery Targeting Focal Adhesion Kinase (FAK) as a Promising Cancer Therapy
Molecules 2021 Jul 13;26(14):4250.PMID:34299525DOI:10.3390/molecules26144250.
FAK is a nonreceptor intracellular tyrosine kinase which plays an important biological function. Many studies have found that FAK is overexpressed in many human cancer cell lines, which promotes tumor cell growth by controlling cell adhesion, migration, proliferation, and survival. Therefore, targeting FAK is considered to be a promising cancer therapy with small molecules. Many FAK inhibitors have been reported as anticancer agents with various mechanisms. Currently, six FAK inhibitors, including GSK-2256098 (Phase I), VS-6063 (Phase II), CEP-37440 (Phase I), VS-6062 (Phase I), VS-4718 (Phase I), and BI-853520 (Phase I) are undergoing clinical trials in different phases. Up to now, there have been many novel FAK inhibitors with anticancer activity reported by different research groups. In addition, FAK degraders have been successfully developed through "proteolysis targeting chimera" (PROTAC) technology, opening up a new way for FAK-targeted therapy. In this paper, the structure and biological function of FAK are reviewed, and we summarize the design, chemical types, and activity of FAK inhibitors according to the development of FAK drugs, which provided the reference for the discovery of new anticancer agents.